Therapeutic composition



Patented Apr. 25, 1939 UNIT D STATES THERAPEUTIC COMPOSITION John B. Wright, Larchmont, N. r., assignor to Piedmont Development Corporation, Wilmintton, lleL, a corporation of Delaware No Drawing. Application October 29,1931, Serial No. 171,688

Claim8. (Cl. 167-58) This invention relates to new compositions adapted'for use as nose drops or nasal sprays in the treatment of head colds and the like. It relates more particularly to new compositions for 5 this purpose having an aqueous base and containing a suitable verso-constricting agent or agents, local anaesthetics, analgesics, aromatic materials, etc., and in addition to such conventional constituents, a small amount of polyvinyl alcohol to give a controlled increase in viscosity. The nature of the compositions is such that they have a viscosity which does not change greatly in the 'temperature range from about 40 F. to about 100 F.; and the compositions have a relatively 10 high viscosity at nasal temperatures such that they spread readily over the surfaces of the mucous membranes on contact and remain in contact with them, while at lower temperatures their viscosity is not. so great as to preclude ready to administration with a dropping device or spray. It has heretofore been proposed to prepare nose drops or sprays in the form of aqueous solutions of vase-constricting agents such as water soluble salts ofephedrine, epinephrine. or other vasoq g5 constrictor amines, together with other materials, such as suitable antisepticsfaromatic materials,

analgesics, local anaesthetics, etc.; but in general these compositions are subject to serious disadvantages in that their viscosity issuch that they 30 do not spread effectively over the surfaces of the mucous membranes on contact, nor remain in contact with them for a suillcient period of time to perform their function effectively.

In accordance with the present invention, com

35 positions adapted for use as nose drops or sprays are provided which have an aqueous base, and which contain, in addition to 'more or less conventional ingredients, a relatively small amount of polyvinyl alcohol. The polyvinyl alcohol, in

40 the quantities used, has the property of increas ing the viscosity of the compositions at nasal temperatures to an extent such. that the compositions readily spread upon contact with the mucous membranes and remain in contact with 5 them, thus having increased therapeutic efliciency, without increasing the viscosity at room temperatures or temperatures below room temperature, e. g. as low as 40'' 'F.,'B0 such an extent as to cause the compositions to gel or to preclude 50 their ready administration with spray or dropping devices. It is an important advantage of polyvinyl alcohol that the change in viscosity of such aqueous compositions, with temperature, at least in the temperature range of from about 40 F.

5 to about 100 F., is not particularly great, so that an aqueous solution suitable for use as a nasal spray or nose drop having a relative viscosity,

at nasal temperatures, of about 4 to 5, as compared to water, as determined by the use of a Dudleypipette, is still sufliciently fluid at tem- 5 peratures down as low as 40 F. to be readily administered. While the viscosity of the compositions both at nasal temperatures and lower temperatures may be varied over relatively wide ranges, I have found it advantageous to use an 10 amount of polyvinyl alcohol which will imparts. relative viscosity at nasal temperatures of about 4 to about 5, as determined by the Dudley pipette, the relatively uniform viscosity over the temperature range of about 40 F. to 100 F. insuring .15 a-suiiiciently low viscosity at lower temperatures to permit ready administration.

Polyvinyl alcohol has the further advantages that it is very stable in the presence of water and other ingredients used in nose drops and nasal sprays, even under slightly acid or alkaline conditions, and is compatible with the other constituents of the compositions. Furthermore, it is extremely resistant to putrefactive and fermentative changes, and need not be used in large con- 26 centrations such as might result in the deposition of objectionable residues in the nasal passages.

It is non-irritating.

In general, the amount of polyvinyl alcohol which may be used with advantage isabout 3.5% 30 or somewhat more of the total composition; such amount of polyvinyl alcohol,'when incorporated in the aqueous base, increasing the relative viscosity of the compositions at nasal temperatures a to about 4 to 5 as determined by the Dudley pipette and-resulting in a composition which has a relatively uniform viscosity over the temperature range from about 40 F. to about 100 F. and is sufllciently fluid at the lower temperatures to permit ready administration. It will be ap- 4o preciated that the amount of polyvinyl alcohol used must be varied to make allowance for variations in properties of the polyvinyl alcohol, as certain polyvinyl alcohols produce the desired increase in viscosity in lesser amounts than others. In any case, it is a simple matter to determine how much of a particular grade or batch must be used to produce the desired increase in viscosity.

The invention will be further illustrated by so the following specific example, but it is not limited thereto:

An aqueous solution containing about 1% of ephedrine sulfate, 05% of chlorbutanol, 0.85% of sodium chloride and about 3.5% of polyvinyl alis PETS 01' sprays.

cohol is prepared. The resulting composition is approximately isotonic and has a sufliciently high relative viscosity, i. e., about 4 to 5 as measured by the Dudley pipette, at nasal temperatures so that it spreads readily upon contact with the mucous membranes and remains in contact with them, thus being highly effective for the treatment of head colds and the like. At the same time, its viscosity at lower temperatures, e. g., down to 40 F. is sufilciently low so that it can be readily administered with nose drop- If desired, one or more of the aromatics, such as thymol, menthol, eucalyptol, etc., may be added up to saturation to make the composition more pleasant when administered.

The ephedrine sulfate in the composition of the example is a vase-constricting agent, and is the therapeutically efiective ingredient. It may, of course, be replaced by other salts of ephedrine, such as the hydrochloride, or by other suitable water soluble vaso-constricting agents of the same general nature, such as water soluble salts of epinephrine, phenyl and hydroxy-phenyl propanol amines, phenyl and hydroxylphenyl ethanol amines, etc. The chlorbutanol is an analgesic, local anaesthetic and antiseptic, and may be omitted or replaced by other suitable' analgesics, local anaesthetic or antiseptics. If desired, the compositions may be varied by the inclusion of other ingredients, the present invention being directed to the use of the polyvinyl alcohol for the proper control of the viscosity of the aqueous base compositions at nasal and lower temperatures. I

I claim: 1. An aqueous composition adapted for use as nose drops or nasal sprays including, in addition to therapeutic ingredients, a small amount of polyvinyl alcohol.

2. An aqueous composition adapted for use as nose drops or nasal sprays containing a vaso-constricting agent'and a small amount of polyvinyl alcohol. 3. An aqueous composition adapted for use as -nose drops or nasal sprays containing a salt 

